Page last updated: 2024-11-11

cefpodoxime

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Description

4-(6-methoxy-2-naphthyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazole: a Tie2 kinase inhibitor with antineoplastic activity [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23625762
CHEMBL ID237352
CHEBI ID91442
SCHEMBL ID17835458
MeSH IDM0150936
PubMed CID6335986
CHEMBL ID1672
CHEBI ID3504
SCHEMBL ID27072
MeSH IDM0150936

Synonyms (89)

Synonym
CHEMBL237352 ,
4-(4-(6-methoxynaphthalen-2-yl)-2-(4-(methylsulfinyl)phenyl)-1h-imidazol-5-yl)pyridine
bdbm50217603
4-[2-(4-methanesulfinylphenyl)-5-(6-methoxynaphthalen-2-yl)-1h-imidazol-4-yl]pyridine
FT-0671288
948557-43-5
TIE2 KINASE INHIBITOR ,
NCGC00346554-01
smr004702865
MLS006011077
compound 5 [pmid: 17618114]
gtpl9348
SCHEMBL17835458
DTXSID60635231
4-[4-(6-methoxynaphthalen-2-yl)-2-(4-methylsulfinylphenyl)-1h-imidazol-5-yl]pyridine
CHEBI:91442
HMS3655I07
NCGC00386151-02
SW219921-1
tie2 in 5; tie2in5; tie2 inhibitor 5; tie2-inhibitor-5; tie2 kinase inhibitor 5
tie2-in-5
BCP23755
4-[4-(6-methoxy-2-naphthalenyl)-2-(4-methylsulfinylphenyl)-1h-imidazol-5-yl]pyridine
Q27163288
4-[4-(6-methoxy-2-naphthalenyl)-2-[4-(methylsulfinyl)phenyl]-1h-imidazol-5-yl]pyridine
EX-A7310
S1577
HY-100556
tie2 kinase inhibitor 1
CS-0019702
HMS3672K19
CCG-264916
tie2 kinase-in-1
A917005
tie-2 kinase inhibitor
AS-56742
4-(6-methoxy-2-naphthyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1h-imidazole
AKOS037515690
tie2kinase-in-1
tie2 kinase
(6r,7r)-7-({(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[(methyloxy)imino]acetyl}amino)-3-[(methyloxy)methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
D07650
epoxim (tn)
cpdx
cefpodoxime (inn)
C08114 ,
DB01416
cefpodoximum [latin]
cefpodoxime [inn:ban]
5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-(((2-amino-4-thiazolyl)(methoxyimino)acetyl)amino)-3-(methoxymethyl)-8-oxo-, (6r-(6alpha,7beta(z)))-
cefpodoxima [spanish]
cefpodoxima
(6r,7r)-7-{[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino}-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
CHEBI:3504 ,
cefpodoximum
7beta-[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido]-3-(methoxymethyl)-3,4-didehydrocepham-4-carboxylic acid
(6r,7r)-7-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
epoxim
CHEMBL1672 ,
4-{((r)-2-carboxy-3-methoxymethyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-en-7-ylcarbamoyl)-[(z)-methoxyimino]-methyl}-thiazol-2-yl-ammonium
bdbm50292251
unii-7r4f94tvgy
7r4f94tvgy ,
AKOS016008786
ru 51807
cefpodoxime, free acid
cefpodoxime proxetil impurity a [ep impurity]
(+)-(6r,7r)-7-(2-(2-amino-4-thiazolyl)-2-((z)-methoxyimino)acetamido)-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid
cefpodoxime [jan]
(+)-(6r,7r)-7-(2-(2-amino-4-thiazolyl)glyoxylamido)-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7(sup 2)-(z)-(o-methyloxime)
cefpodoxime [inn]
cefpodoxime [mi]
cefpodoxime [who-dd]
SCHEMBL27072
DTXSID6022765 ,
(6r,7r)-7-[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido]-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
SR-01000872579-1
sr-01000872579
cefpodoxime, vetranal(tm), analytical standard
mfcd00864906
NCGC00532497-01
MS-27549
EN300-22411570
HY-A0251
CS-0017595
dtxcid402765
(6r,7r)-7-(((2z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl)amino)-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid
cefpodoximum (latin)
7beta-((2z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido)-3-(methoxymethyl)-3,4-didehydrocepham-4-carboxylic acid

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"The utilization of the membrane transport protein PEPT1 as a drug delivery system is a promising strategy to enhance the oral bioavailability of drugs."( Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1.
Biegel, A; Brandsch, M; Gebauer, S; Hartrodt, B; Neubert, K; Thondorf, I, 2005
)
0.33
" Reported here is a novel, orally bioavailable diazabicyclooctane (DBO) β-lactamase inhibitor."( Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
Carter, NM; Chen, A; Chen, Y; Comita-Prevoir, J; Durand-Réville, TF; Giacobbe, RA; Lahiri, SD; May-Dracka, TL; McLeod, SM; Miller, AA; Mueller, JP; O'Donnell, JP; Romero, JAC; Sacco, MD; Shapiro, AB; Tommasi, RA; Verheijen, JC; Wu, F; Wu, X; Zhang, J, 2020
)
0.56

Dosage Studied

ExcerptRelevanceReference
" adipose tissue met the efficacy breakpoint (percentage of the time that free drug concentrations remained above the MIC) for at least 40% of the 8-h dosing interval for organisms with a MIC of 2 mg/liter."( Soft-tissue penetration of ceftobiprole in healthy volunteers determined by in vivo microdialysis.
Barbour, A; Derendorf, H; Grant, M; Murthy, B; Sabarinath, SN; Schmidt, S; Seubert, C; Skee, D, 2009
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
antibacterial drugA drug used to treat or prevent bacterial infections.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
imidazolesA five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
cephalosporinA class of beta-lactam antibiotics differing from the penicillins in having a 6-membered, rather than a 5-membered, side ring. Although cephalosporins are among the most commonly used antibiotics in the treatment of routine infections, and their use is increasing over time, they can cause a range of hypersensitivity reactions, from mild, delayed-onset cutaneous reactions to life-threatening anaphylaxis in patients with immunoglobulin E (IgE)-mediated allergy.
carboxylic acidA carbon oxoacid acid carrying at least one -C(=O)OH group and having the structure RC(=O)OH, where R is any any monovalent functional group. Carboxylic acids are the most common type of organic acid.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency33.17340.00308.794948.0869AID1347053
PPM1D proteinHomo sapiens (human)Potency46.61280.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.42530.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency26.70140.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
GVesicular stomatitis virusPotency3.37860.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency3.37860.00108.379861.1304AID1645840
polyproteinZika virusPotency33.17340.00308.794948.0869AID1347053
Interferon betaHomo sapiens (human)Potency35.80430.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Angiopoietin-1 receptorHomo sapiens (human)IC50 (µMol)10.12500.00040.55539.0700AID300639; AID301530
Solute carrier family 15 member 1Homo sapiens (human)Ki30,000.00000.18003.39339.8000AID238858
Solute carrier family 15 member 2Homo sapiens (human)Ki30,951.50000.79434.22108.0000AID612540
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (95)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAngiopoietin-1 receptorHomo sapiens (human)
angiogenesisAngiopoietin-1 receptorHomo sapiens (human)
response to hypoxiaAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of protein phosphorylationAngiopoietin-1 receptorHomo sapiens (human)
endothelial cell proliferationAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of endothelial cell proliferationAngiopoietin-1 receptorHomo sapiens (human)
endochondral ossificationAngiopoietin-1 receptorHomo sapiens (human)
sprouting angiogenesisAngiopoietin-1 receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayAngiopoietin-1 receptorHomo sapiens (human)
cell-cell signalingAngiopoietin-1 receptorHomo sapiens (human)
heart developmentAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of endothelial cell migrationAngiopoietin-1 receptorHomo sapiens (human)
negative regulation of angiogenesisAngiopoietin-1 receptorHomo sapiens (human)
regulation of establishment or maintenance of cell polarityAngiopoietin-1 receptorHomo sapiens (human)
substrate adhesion-dependent cell spreadingAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of Rac protein signal transductionAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of Rho protein signal transductionAngiopoietin-1 receptorHomo sapiens (human)
negative regulation of apoptotic processAngiopoietin-1 receptorHomo sapiens (human)
regulation of vascular permeabilityAngiopoietin-1 receptorHomo sapiens (human)
response to peptide hormoneAngiopoietin-1 receptorHomo sapiens (human)
response to estrogenAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of angiogenesisAngiopoietin-1 receptorHomo sapiens (human)
Tie signaling pathwayAngiopoietin-1 receptorHomo sapiens (human)
negative regulation of inflammatory responseAngiopoietin-1 receptorHomo sapiens (human)
response to cAMPAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of focal adhesion assemblyAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionAngiopoietin-1 receptorHomo sapiens (human)
definitive hemopoiesisAngiopoietin-1 receptorHomo sapiens (human)
heart trabecula formationAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAngiopoietin-1 receptorHomo sapiens (human)
glomerulus vasculature developmentAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of intracellular signal transductionAngiopoietin-1 receptorHomo sapiens (human)
regulation of endothelial cell apoptotic processAngiopoietin-1 receptorHomo sapiens (human)
negative regulation of endothelial cell apoptotic processAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of MAPK cascadeAngiopoietin-1 receptorHomo sapiens (human)
positive regulation of kinase activityAngiopoietin-1 receptorHomo sapiens (human)
multicellular organism developmentAngiopoietin-1 receptorHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
monoatomic ion transportSolute carrier family 15 member 1Homo sapiens (human)
protein transportSolute carrier family 15 member 1Homo sapiens (human)
peptide transportSolute carrier family 15 member 1Homo sapiens (human)
dipeptide import across plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
tripeptide import across plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
proton transmembrane transportSolute carrier family 15 member 1Homo sapiens (human)
monoatomic ion transportSolute carrier family 15 member 2Homo sapiens (human)
protein transportSolute carrier family 15 member 2Homo sapiens (human)
peptide transportSolute carrier family 15 member 2Homo sapiens (human)
peptidoglycan transportSolute carrier family 15 member 2Homo sapiens (human)
xenobiotic transportSolute carrier family 15 member 2Homo sapiens (human)
dipeptide transportSolute carrier family 15 member 2Homo sapiens (human)
renal absorptionSolute carrier family 15 member 2Homo sapiens (human)
regulation of nucleotide-binding domain, leucine rich repeat containing receptor signaling pathwaySolute carrier family 15 member 2Homo sapiens (human)
dipeptide import across plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
tripeptide import across plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
antibacterial innate immune responseSolute carrier family 15 member 2Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 15 member 2Homo sapiens (human)
proton transmembrane transportSolute carrier family 15 member 2Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein kinase activityAngiopoietin-1 receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityAngiopoietin-1 receptorHomo sapiens (human)
protein bindingAngiopoietin-1 receptorHomo sapiens (human)
ATP bindingAngiopoietin-1 receptorHomo sapiens (human)
growth factor bindingAngiopoietin-1 receptorHomo sapiens (human)
signaling receptor activityAngiopoietin-1 receptorHomo sapiens (human)
identical protein bindingAngiopoietin-1 receptorHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
proton-dependent oligopeptide secondary active transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
peptide:proton symporter activitySolute carrier family 15 member 1Homo sapiens (human)
tripeptide transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
dipeptide transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
protein bindingSolute carrier family 15 member 2Homo sapiens (human)
peptide:proton symporter activitySolute carrier family 15 member 2Homo sapiens (human)
tripeptide transmembrane transporter activitySolute carrier family 15 member 2Homo sapiens (human)
dipeptide transmembrane transporter activitySolute carrier family 15 member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (34)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
stress fiberAngiopoietin-1 receptorHomo sapiens (human)
actin filamentAngiopoietin-1 receptorHomo sapiens (human)
extracellular regionAngiopoietin-1 receptorHomo sapiens (human)
cytoplasmAngiopoietin-1 receptorHomo sapiens (human)
plasma membraneAngiopoietin-1 receptorHomo sapiens (human)
microvillusAngiopoietin-1 receptorHomo sapiens (human)
cell-cell junctionAngiopoietin-1 receptorHomo sapiens (human)
focal adhesionAngiopoietin-1 receptorHomo sapiens (human)
basal plasma membraneAngiopoietin-1 receptorHomo sapiens (human)
cell surfaceAngiopoietin-1 receptorHomo sapiens (human)
basolateral plasma membraneAngiopoietin-1 receptorHomo sapiens (human)
apical plasma membraneAngiopoietin-1 receptorHomo sapiens (human)
centriolar satelliteAngiopoietin-1 receptorHomo sapiens (human)
membrane raftAngiopoietin-1 receptorHomo sapiens (human)
plasma membraneAngiopoietin-1 receptorHomo sapiens (human)
receptor complexAngiopoietin-1 receptorHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
brush borderSolute carrier family 15 member 1Homo sapiens (human)
membraneSolute carrier family 15 member 1Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
phagocytic vesicle membraneSolute carrier family 15 member 2Homo sapiens (human)
plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
membraneSolute carrier family 15 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
extracellular exosomeSolute carrier family 15 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (204)

Assay IDTitleYearJournalArticle
AID300645Reduction in bFGF-induced angiogenesis in Matrigel mouse model at 25 mg/kg, ip bid2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pyridinylimidazole inhibitors of Tie2 kinase.
AID300641Selectivity of Tie2 over VEGFR22007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pyridinylimidazole inhibitors of Tie2 kinase.
AID300644Efficacy in mouse MOPC315 cells xenografted mouse assessed as delay in tumor growth2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pyridinylimidazole inhibitors of Tie2 kinase.
AID301530Inhibition of Tie22007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Optimization of triarylimidazoles for Tie2: influence of conformation on potency.
AID300642Selectivity of Tie2 over VEGFR32007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pyridinylimidazole inhibitors of Tie2 kinase.
AID300643Selectivity of Tie2 over PDGFR1beta2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pyridinylimidazole inhibitors of Tie2 kinase.
AID300646Reduction in bFGF-induced angiogenesis in Matrigel mouse model at 50 mg/kg, ip bid2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pyridinylimidazole inhibitors of Tie2 kinase.
AID300640Inhibition of P38 kinase2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pyridinylimidazole inhibitors of Tie2 kinase.
AID300639Inhibition of Tie2 kinase by autophosphorylation assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pyridinylimidazole inhibitors of Tie2 kinase.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347149Furin counterscreen qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347169Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347153Confirmatory screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347167Vero cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347168HepG2 cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347161Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347152Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1345549Human TEK receptor tyrosine kinase (Type XII RTKs: TIE family of angiopoietin receptors)2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Pyridinylimidazole inhibitors of Tie2 kinase.
AID560051Antibacterial activity against Neisseria gonorrhoeae isolate SM4 expressing SF-B mosaic penA allele by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mosaic penicillin-binding protein 2 in Neisseria gonorrhoeae isolates collected in 2008 in San Francisco, California.
AID1740635Antibacterial activity against Escherichia coli ARC 6078 drug resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID558631Antimicrobial activity against Streptococcus pneumoniae isolate 4755 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID558630Antimicrobial activity against Streptococcus pneumoniae isolate 4747 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID558600Antimicrobial activity against Streptococcus pneumoniae 12 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID562774Antimicrobial activity against Escherichia coli DH10B by disk diffusion method in presence of clavulanic acid2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID1740670In vivo antibacterial activity against multidrug-resistant Escherichia coli ARC 2687 infected in CD-1 mouse model of neutropenic thigh infection assessed as colony forming unit at 50 mg/kg, po administered at 6 hrs interval2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID558610Antimicrobial activity against Streptococcus pneumoniae isolate 1424 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID560770Antibacterial activity against Neisseria gonorrhoeae isolate SW1 expressing nonmosaic penA allele by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mosaic penicillin-binding protein 2 in Neisseria gonorrhoeae isolates collected in 2008 in San Francisco, California.
AID558612Antimicrobial activity against Streptococcus pneumoniae isolate 2617 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID612540Binding affinity to human PepT2 in SKTP cells2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Fragmental modeling of hPepT2 and analysis of its binding features by docking studies and pharmacophore mapping.
AID372553Antibacterial activity against genetically beta-lactamase-negative ampicillin-susceptible Haemophilus influenzae type b without amino acid substitutions in ftsI gene and bla gene assessed as susceptibility rate by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Genetic characteristics and clonal dissemination of beta-lactamase-negative ampicillin-resistant Haemophilus influenzae strains isolated from the upper respiratory tract of patients in Japan.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1740641Antibacterial activity against Citrobacter freundii ARC 3518 carbapenem resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID558626Antimicrobial activity against Streptococcus pneumoniae isolate 3481 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID560771Antibacterial activity against Neisseria gonorrhoeae isolate SW2 expressing nonmosaic penA allele by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mosaic penicillin-binding protein 2 in Neisseria gonorrhoeae isolates collected in 2008 in San Francisco, California.
AID372559Antibacterial activity against genetically beta-lactamase-negative ampicillin-susceptible Haemophilus influenzae type b without amino acid substitutions in ftsI gene and bla gene assessed as resistance rate by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Genetic characteristics and clonal dissemination of beta-lactamase-negative ampicillin-resistant Haemophilus influenzae strains isolated from the upper respiratory tract of patients in Japan.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID558619Antimicrobial activity against Streptococcus pneumoniae isolate 3275 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID530288Antimicrobial activity against PR-39-resistant Salmonella enterica serovar Typhimurium LT2 DA6192 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mechanism and fitness costs of PR-39 resistance in Salmonella enterica serovar Typhimurium LT2.
AID372547Antibacterial activity against genetically beta-lactamase-negative ampicillin-susceptible Haemophilus influenzae type b without amino acid substitutions in ftsI gene and bla gene by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Genetic characteristics and clonal dissemination of beta-lactamase-negative ampicillin-resistant Haemophilus influenzae strains isolated from the upper respiratory tract of patients in Japan.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID521325Antimicrobial activity against beta lactamase-nonproducing ampicillin-resistant Haemophilus influenzae MSC06663 isolate harboring Met377Ile, Ser385Thr and Asn526Lys mutations in penicillin-binding protein 3 by broth dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the efficacies of oral beta-lactams in selection of Haemophilus influenzae transformants with mutated ftsI genes.
AID558583Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558582Antimicrobial activity against penicillin-intermediate Streptococcus pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID562773Antimicrobial activity against Escherichia coli DH10B by disk diffusion method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID558597Antimicrobial activity against Streptococcus pneumoniae 9 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID558616Antimicrobial activity against Streptococcus pneumoniae isolate 2880 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID558628Antimicrobial activity against Streptococcus pneumoniae isolate 3681 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558596Antimicrobial activity against Streptococcus pneumoniae 8 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID656363Plasma protein binding in human2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Preparation, gram-negative antibacterial activity, and hydrolytic stability of novel siderophore-conjugated monocarbam diols.
AID558624Antimicrobial activity against Streptococcus pneumoniae isolate 3455 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID543427Antimicrobial activity against Escherichia coli XL-1 Blue harboring plasmid CL1920 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Novel chimeric beta-lactamase CTX-M-64, a hybrid of CTX-M-15-like and CTX-M-14 beta-lactamases, found in a Shigella sonnei strain resistant to various oxyimino-cephalosporins, including ceftazidime.
AID543411Antimicrobial activity against Shigella sonnei UIH-1 expressing beta-lactamase CTX-M-64 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Novel chimeric beta-lactamase CTX-M-64, a hybrid of CTX-M-15-like and CTX-M-14 beta-lactamases, found in a Shigella sonnei strain resistant to various oxyimino-cephalosporins, including ceftazidime.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1740632Antibacterial activity against Escherichia coli ARC 6059 drug resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID558615Antimicrobial activity against Streptococcus pneumoniae isolate 2874 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID560049Antibacterial activity against Neisseria gonorrhoeae isolate SM2 expressing SF-A mosaic penA allele by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mosaic penicillin-binding protein 2 in Neisseria gonorrhoeae isolates collected in 2008 in San Francisco, California.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID558613Antimicrobial activity against Streptococcus pneumoniae isolate 2686 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1740633Antibacterial activity against Escherichia coli ARC 6064 drug resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID535691Antimicrobial activity against beta-lactamase CTX-M-15-producing fluoroquinolone-resistant Escherichia coli FMV5825 expressing qnrB2 and aac(6')-Ib-cr and harboring gyrA Ser83Ile and Asp87Asn mutant gene and ParC Ser80Ile and Glu84Val mutant gene obtained2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Detection of the pandemic O25-ST131 human virulent Escherichia coli CTX-M-15-producing clone harboring the qnrB2 and aac(6')-Ib-cr genes in a dog.
AID372548Antibacterial activity against genetically beta-lactamase-negative ampicillin-resistant Haemophilus influenzae type b with an amino acid substitution in variable mutated locus Asn-526 or Arg-517 of ftsI gene by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Genetic characteristics and clonal dissemination of beta-lactamase-negative ampicillin-resistant Haemophilus influenzae strains isolated from the upper respiratory tract of patients in Japan.
AID562766Antimicrobial activity against Escherichia coli DH10B transformant harboring blaTEM-168 gene by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID558623Antimicrobial activity against Streptococcus pneumoniae isolate 3412 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID438297Inhibition of penicillin-sensitive Streptococcus pneumoniae R6 PBP2X preincubated for 1 hr before addition of substrate (R)-[2-(benzoylamino)propionylsulfanyl]acetic acid2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Discovery of new inhibitors of resistant Streptococcus pneumoniae penicillin binding protein (PBP) 2x by structure-based virtual screening.
AID558590Antimicrobial activity against Streptococcus pneumoniae 2 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID558607Antimicrobial activity against Streptococcus pneumoniae isolate 1384 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558606Antimicrobial activity against Streptococcus pneumoniae isolate 1147 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID521324Antimicrobial activity against beta lactamase-nonproducing ampicillin-resistant Haemophilus influenzae MSC06647 isolate harboring Asn526Lys mutation in penicillin-binding protein 3 by broth dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the efficacies of oral beta-lactams in selection of Haemophilus influenzae transformants with mutated ftsI genes.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID558591Antimicrobial activity against Streptococcus pneumoniae 3 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558581Antimicrobial activity against penicillin-susceptible Streptococcus pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID562765Antimicrobial activity against Escherichia coli DH10B transformant harboring blaTEM-168 gene by disk diffusion method in presence of clavulanic acid2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID558587Antimicrobial activity against Streptococcus pneumoniae 19A by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID558604Antimicrobial activity against Streptococcus pneumoniae isolate 1055 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1740636Antibacterial activity against Klebsiella pneumoniae ARC 6082 drug resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID1740609Antibacterial activity against Escherichia coli ARC3627 assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID558617Antimicrobial activity against Streptococcus pneumoniae isolate 3260 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558602Antimicrobial activity against Streptococcus pneumoniae isolate 33 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558625Antimicrobial activity against Streptococcus pneumoniae isolate 3458 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID530287Antimicrobial activity against PR-39-resistant sbmA-deficient Salmonella enterica serovar Typhimurium LT2 DA12088 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mechanism and fitness costs of PR-39 resistance in Salmonella enterica serovar Typhimurium LT2.
AID558595Antimicrobial activity against Streptococcus pneumoniae 7 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1740638Antibacterial activity against Klebsiella pneumoniae ARC 6098 drug resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID530286Antimicrobial activity against PR-39-resistant Salmonella enterica serovar Typhimurium LT2 DA10899 harboring Q179Stop mutant gene by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mechanism and fitness costs of PR-39 resistance in Salmonella enterica serovar Typhimurium LT2.
AID558594Antimicrobial activity against Streptococcus pneumoniae 6 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID558608Antimicrobial activity against Streptococcus pneumoniae isolate 1394 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID562775Antimicrobial activity against Escherichia coli DH10B by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID372549Antibacterial activity against genetically beta-lactamase-negative ampicillin-resistant Haemophilus influenzae type b with an amino acid substitution in highly mutated locus Ser-385 of ftsI gene by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Genetic characteristics and clonal dissemination of beta-lactamase-negative ampicillin-resistant Haemophilus influenzae strains isolated from the upper respiratory tract of patients in Japan.
AID1740643Antibacterial activity against Enterobacter cloacae ARC 6055 drug resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID1740639Antibacterial activity against Klebsiella pneumoniae ARC 6107 carbapenem resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID561807fAUC in plasma of healthy human at 400 mg, po by microdialysis2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Soft-tissue penetration of ceftobiprole in healthy volunteers determined by in vivo microdialysis.
AID558603Antimicrobial activity against Streptococcus pneumoniae isolate 37 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558618Antimicrobial activity against Streptococcus pneumoniae isolate 3263 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID562574Antimicrobial activity against Escherichia coli NO8-1503 harboring blaTEM-168 gene by disk diffusion method in presence of clavulanic acid2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID558598Antimicrobial activity against Streptococcus pneumoniae 10 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1740642Antibacterial activity against Enterobacter cloacae ARC 6049 drug resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID372555Antibacterial activity against genetically beta-lactamase-negative ampicillin-resistant Haemophilus influenzae type b with an amino acid substitution in highly mutated locus Ser-385 of ftsI gene assessed as susceptibility rate by broth microdilution metho2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Genetic characteristics and clonal dissemination of beta-lactamase-negative ampicillin-resistant Haemophilus influenzae strains isolated from the upper respiratory tract of patients in Japan.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1740631Antibacterial activity against Escherichia coli ARC 2687 drug resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1740637Antibacterial activity against Klebsiella pneumoniae ARC 6088 carbapenem-resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID558620Antimicrobial activity against Streptococcus pneumoniae isolate 3282 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558609Antimicrobial activity against Streptococcus pneumoniae isolate 1397 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558629Antimicrobial activity against Streptococcus pneumoniae isolate 3791 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID561806AUC in plasma of healthy human at 400 mg, po by microdialysis2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Soft-tissue penetration of ceftobiprole in healthy volunteers determined by in vivo microdialysis.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID372561Antibacterial activity against genetically beta-lactamase-negative ampicillin-resistant Haemophilus influenzae type b with an amino acid substitution in highly mutated locus Ser-385 of ftsI gene assessed as resistance rate by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Genetic characteristics and clonal dissemination of beta-lactamase-negative ampicillin-resistant Haemophilus influenzae strains isolated from the upper respiratory tract of patients in Japan.
AID562573Antimicrobial activity against Escherichia coli NO8-1503 harboring blaTEM-168 gene by disk diffusion method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID372560Antibacterial activity against genetically beta-lactamase-negative ampicillin-resistant Haemophilus influenzae type b with an amino acid substitution in variable mutated locus Asn-526 or Arg-517 of ftsI gene assessed as resistance rate by broth microdilut2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Genetic characteristics and clonal dissemination of beta-lactamase-negative ampicillin-resistant Haemophilus influenzae strains isolated from the upper respiratory tract of patients in Japan.
AID543419Antimicrobial activity against rifampicin-resistant Escherichia coli X1037 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Novel chimeric beta-lactamase CTX-M-64, a hybrid of CTX-M-15-like and CTX-M-14 beta-lactamases, found in a Shigella sonnei strain resistant to various oxyimino-cephalosporins, including ceftazidime.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID372554Antibacterial activity against genetically beta-lactamase-negative ampicillin-resistant Haemophilus influenzae type b with an amino acid substitution in variable mutated locus Asn-526 or Arg-517 of ftsI gene assessed as susceptibility rate by broth microd2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Genetic characteristics and clonal dissemination of beta-lactamase-negative ampicillin-resistant Haemophilus influenzae strains isolated from the upper respiratory tract of patients in Japan.
AID1740640Antibacterial activity against Klebsiella oxytoca ARC 5389 carbapenem resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID562776Antimicrobial activity against Escherichia coli DH10B by broth microdilution method in presence of clavulanic acid2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID562575Antimicrobial activity against Escherichia coli NO8-1503 harboring blaTEM-168 gene by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID561808fAUC in muscle of healthy human at 400 mg, po by microdialysis2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Soft-tissue penetration of ceftobiprole in healthy volunteers determined by in vivo microdialysis.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID562767Antimicrobial activity against Escherichia coli DH10B transformant harboring blaTEM-168 gene by broth microdilution method in presence of clavulanic acid2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID1740634Antibacterial activity against Escherichia coli ARC 6077 drug resistant clinical isolates assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID558593Antimicrobial activity against Streptococcus pneumoniae 5 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558621Antimicrobial activity against Streptococcus pneumoniae isolate 3346 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID562764Antimicrobial activity against Escherichia coli DH10B transformant harboring blaTEM-168 gene by disk diffusion method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID558592Antimicrobial activity against Streptococcus pneumoniae 4 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID521323Antimicrobial activity against rifampin-resistant Haemophilus influenzae Rd clone by broth dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the efficacies of oral beta-lactams in selection of Haemophilus influenzae transformants with mutated ftsI genes.
AID560050Antibacterial activity against Neisseria gonorrhoeae isolate SM3 expressing SF-A mosaic penA allele by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mosaic penicillin-binding protein 2 in Neisseria gonorrhoeae isolates collected in 2008 in San Francisco, California.
AID543415Antimicrobial activity against rifampicin-resistant Escherichia coli X1037 transconjugant by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Novel chimeric beta-lactamase CTX-M-64, a hybrid of CTX-M-15-like and CTX-M-14 beta-lactamases, found in a Shigella sonnei strain resistant to various oxyimino-cephalosporins, including ceftazidime.
AID558611Antimicrobial activity against Streptococcus pneumoniae isolate 1564 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558605Antimicrobial activity against Streptococcus pneumoniae isolate 1146 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID438298Inhibition of penicillin-resistant Streptococcus pneumoniae 5204 PBP2X preincubated for 4 hrs before addition of substrate (R)-[2-(benzoylamino)propionylsulfanyl]acetic acid2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Discovery of new inhibitors of resistant Streptococcus pneumoniae penicillin binding protein (PBP) 2x by structure-based virtual screening.
AID558589Antimicrobial activity against Streptococcus pneumoniae 1 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558599Antimicrobial activity against Streptococcus pneumoniae 11 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID558614Antimicrobial activity against Streptococcus pneumoniae isolate 2688 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558627Antimicrobial activity against Streptococcus pneumoniae isolate 3587 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID543423Antimicrobial activity against Escherichia coli XL-1 Blue transconjugant harboring beta-lactamase CTX-M-64 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Novel chimeric beta-lactamase CTX-M-64, a hybrid of CTX-M-15-like and CTX-M-14 beta-lactamases, found in a Shigella sonnei strain resistant to various oxyimino-cephalosporins, including ceftazidime.
AID1740610Antibacterial activity against Klebsiella pneumoniae ARC561 assessed as reduction in bacterial growth by CLSI based broth dilution method2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases.
AID535694Antimicrobial activity against Azide-resistant Escherichia coli J53 transconjugant harboring Escherichia coli DH5alpha-5825 qnrB2 gene by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Detection of the pandemic O25-ST131 human virulent Escherichia coli CTX-M-15-producing clone harboring the qnrB2 and aac(6')-Ib-cr genes in a dog.
AID562576Antimicrobial activity against Escherichia coli NO8-1503 harboring blaTEM-168 gene by broth microdilution method in presence of clavulanic acid2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
AID561809Ratio of fAUC in muscle to fAUC in plasma of healthy human at 400 mg, po by microdialysis2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Soft-tissue penetration of ceftobiprole in healthy volunteers determined by in vivo microdialysis.
AID558622Antimicrobial activity against Streptococcus pneumoniae isolate 3374 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558601Antimicrobial activity against Streptococcus pneumoniae isolate 24 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID238858Binding affinity against membrane transport protein PEPT1 in human Caco-2 cells2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID560048Antibacterial activity against Neisseria gonorrhoeae isolate SM1 expressing SF-A mosaic penA allele by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mosaic penicillin-binding protein 2 in Neisseria gonorrhoeae isolates collected in 2008 in San Francisco, California.
AID560052Antibacterial activity against Neisseria gonorrhoeae isolate SM5 expressing SF-B mosaic penA allele by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mosaic penicillin-binding protein 2 in Neisseria gonorrhoeae isolates collected in 2008 in San Francisco, California.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID535697Antimicrobial activity against Azide-resistant Escherichia coli J53 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Detection of the pandemic O25-ST131 human virulent Escherichia coli CTX-M-15-producing clone harboring the qnrB2 and aac(6')-Ib-cr genes in a dog.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (28)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's14 (50.00)29.6817
2010's7 (25.00)24.3611
2020's7 (25.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 105.14

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index105.14 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.35 (4.65)
Search Engine Demand Index201.55 (26.88)
Search Engine Supply Index2.16 (0.95)

This Compound (105.14)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials1 (5.56%)5.53%
Reviews0 (0.00%)6.00%
Reviews1 (5.56%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other11 (100.00%)84.16%
Other16 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (11)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics [NCT02099240]Early Phase 111 participants (Actual)Interventional2014-03-06Terminated(stopped due to Not enough patient enrollment and lack of staffing)
A Phase 1, Double-Blind, Randomized, Placebo-Controlled Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Oral ETX0282 Administered in Healthy Subjects [NCT03491748]Phase 199 participants (Actual)Interventional2018-03-16Completed
Comparing Oral Versus Parenteral Antimicrobial Therapy (COPAT) Trial [NCT05977868]Phase 4135 participants (Anticipated)Interventional2023-08-04Enrolling by invitation
A Phase One Study of Intravenous Irinotecan and Bortezomib in Children With Recurrent/Refractory High-Risk Neuroblastoma [NCT00644696]Phase 118 participants (Actual)Interventional2008-04-30Completed
A Pilot Study of the Addition of Bevacizumab to Vincristine, Oral Irinotecan, and Temozolomide (VOIT Regimen) for Relapsed/Refractory Pediatric Solid Tumors [NCT00786669]Phase 113 participants (Actual)Interventional2008-10-31Completed
Phase I Study of Intravenous Irinotecan Using Selective Gastrointestinal Decontamination for Prevention of Diarrhea in Relapsed or Refractory Pediatric Solid Tumors [NCT00143533]Phase 120 participants (Actual)Interventional2003-09-30Completed
A Phase I Study of ZD1839 (Iressa) in Combination With Irinotecan (Camptosar or CPT-11) and Vincristine in Pediatric Patients With Refractory Solid Tumors [NCT00186979]Phase 134 participants (Actual)Interventional2003-05-31Completed
Efficacy and Cost Analysis of Steroids in Treatment of Otitis Media With Effusion (OME) Compared to That of Combination of Antibiotic, Antihistaminic, and Nasal Decongestant [NCT03590912]Phase 4160 participants (Actual)Interventional2018-09-05Completed
Nut Allergy Study: Improving Diagnosis And Treatment Of Nut Allergy [NCT01502878]102 participants (Actual)Interventional2011-05-31Completed
Prospective Study Characterizing Fecal Microbiome Disruptions During and After Receipt of Antimicrobials [NCT03098485]20 participants (Actual)Interventional2017-01-31Completed
Cefpodoxime vs Ciprofloxacin for Acute Cystitis [NCT00194532]300 participants (Actual)Interventional2005-06-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00194532 (2) [back to overview]Clinical Cure
NCT00194532 (2) [back to overview]Microbiologic Cure
NCT03098485 (3) [back to overview]Degree of Microbial Disruption: Number of Patients With Continued Microbial Disruption at 185 Days Post-antibiotics
NCT03098485 (3) [back to overview]Degree of Microbial Disruption: Number of Patients With Increase in Antibiotic Resistance Genes at 185 Days Post-antibiotics
NCT03098485 (3) [back to overview]Degree of Microbial Disruption: Number of Patients With Recovery of Bacterial Species Richness at 185 Days Post-antibiotics

Clinical Cure

Participants with clinical cure, i.e. free of urinary tract symptoms and requiring no further antibiotic treatment, to assess the efficacy of a 3-day regimen of cefpodoxime compared to ciprofloxacin (NCT00194532)
Timeframe: 28-30 days post therapy

,
Interventionparticipants (Number)
CureNot cure
Cefpodoxime12327
Ciprofloxacin14010

[back to top]

Microbiologic Cure

Elimination or decrease of causative uropathogen(s) in the mid-stream urine culture at follow-up (NCT00194532)
Timeframe: 1-15 days post therapy

,
Interventionparticipants (Number)
CureNot cure
Cefpodoxime10425
Ciprofloxacin1235

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Degree of Microbial Disruption: Number of Patients With Continued Microbial Disruption at 185 Days Post-antibiotics

The degree of microbiome disruptions will be defined by continuing microbial disruption, as measured by Bray-Curtis dissimilarity, post-antibiotics compared to baseline. (NCT03098485)
Timeframe: Persistent disruption from baseline (7 days prior to antibiotics) in microbial composition at 185 days post-antibiotics

InterventionParticipants (Count of Participants)
Levofloxacin4
Azithromycin4
Cefpodoxime5
Azithromycin and Cefpodoxime5

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Degree of Microbial Disruption: Number of Patients With Increase in Antibiotic Resistance Genes at 185 Days Post-antibiotics

The degree of microbiome disruptions will be defined by an increase in the number of antibiotic resistance genes after antibiotics compared to baseline. (NCT03098485)
Timeframe: Increase from baseline (7 days prior to antibiotics) in antibiotic resistance genes at 185 days post-antibiotics

InterventionParticipants (Count of Participants)
Levofloxacin4
Azithromycin5
Cefpodoxime5
Azithromycin and Cefpodoxime4

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Degree of Microbial Disruption: Number of Patients With Recovery of Bacterial Species Richness at 185 Days Post-antibiotics

The degree of microbial disruption will be defined by recovery of bacterial species richness (number of species) after antibiotics. (NCT03098485)
Timeframe: Decrease from baseline (7 days prior to antibiotics) in microbial diversity at 185 days post-antibiotics

InterventionParticipants (Count of Participants)
Levofloxacin3
Azithromycin3
Cefpodoxime2
Azithromycin and Cefpodoxime3

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